DEVELOPMENT AND EVALUATION OF HYDROGEL OF AN ANTI-FUNGAL DRUG

SAYANTAN BHATTACHARYA, BIPLAB PAUL, GOPA ROY BISWAS
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Abstract

Objective: Topical gel preparations are used for application on skin or to certain mucosal surfaces for local action or for their emollient or protective action. Topical delivery of drugs can be achieved by incorporating drugs into the hydrogel matrix for effective delivery of drugs, thus avoiding first-pass metabolism and for increased local action in pain management and skin diseases. Methods: Hydrogel is a network of polymer chains that are hydrophilic, sometimes found as a colloidal gel in which water is the dispersion medium. Miconazole nitrate (MN) is a broad-spectrum antifungal agent of the imidazole group. It has been selected as a model drug for the preparation of hydrogel. For the preparation of hydrogel, Carbopol of different grades like 934p, 971p, and 974p have been selected. Drug–polymer interaction has been carried out by FT-IR spectroscopy. Standard curve of miconazole nitrate was prepared in phosphate buffer pH 5.5 and 7.4. Physico-chemical characteristics of the hydrogel, like pH, viscosity and % swelling index, were studied. % cumulative drug permeation study through dialysis membrane was done in phosphate buffer pH 7.4. Results: The results were found to be satisfactory. Carbopols have been used in different ratios to get a number of formulations. Out of these, nine formulations have been chosen by their satisfactory physicochemical characteristics and used for the study. The average pH, viscosity, % swelling index and drug content were found to be 7.36, 1.09 x 100 cps, 23.1 and 98.36 %, respectively. Drug permeation kinetics through the dialysis membrane has been done in a Franz diffusion cell at phosphate buffer pH-7.4. The permeation of Miconazole Nitrate through the dialysis membrane was maximum in F1 and minimum in F9. The drug permeation through the dialysis membrane followed zero-order kinetics. Conclusion: A sharp correlation between the % swelling index and the Cumulative % of drug permeated through the dialysis membrane has been found. With the increase in the % swelling index over a period of 6 h the permeation decreased; thus, the swelling of the formulations is responsible to inhibit the permeation of Miconazole Nitrate through the skin.
一种抗真菌药物水凝胶的研制与评价
目的:外用凝胶制剂用于皮肤或某些粘膜表面的局部作用或其润肤或保护作用。局部药物递送可以通过将药物纳入水凝胶基质中来实现,从而有效地递送药物,从而避免首次通过代谢,并增加疼痛管理和皮肤疾病的局部作用。方法:水凝胶是一种亲水性聚合物链的网络,有时被发现为胶体凝胶,其中水是分散介质。硝酸咪康唑(MN)是咪唑类广谱抗真菌药物。它已被选为制备水凝胶的模型药物。制备水凝胶时,选取了934p、971p、974p等不同牌号的卡波波尔。用傅里叶变换红外光谱分析了药物-聚合物相互作用。在pH为5.5和7.4的磷酸盐缓冲液中制备硝酸咪康唑的标准曲线。研究了水凝胶的理化性质,如pH、粘度和%溶胀指数。在pH为7.4的磷酸盐缓冲液中,通过透析膜进行药物累积渗透研究。结果:实验结果令人满意。卡波醇以不同的比例使用,得到了许多配方。从这些配方中,根据其令人满意的理化特性选择了9个配方用于研究。平均pH值为7.36,黏度为1.09 × 100 cps, %溶胀指数为23.1%,药物含量为98.36%。在磷酸缓冲液pH-7.4的Franz扩散池中进行了药物通过透析膜的渗透动力学。硝酸咪康唑通过透析膜的通透性在F1中最大,在F9中最小。药物在透析膜上的渗透遵循零级动力学。结论:溶胀指数与透析膜药物透透率有明显的相关性。随着%溶胀指数的增加,渗透性在6 h内降低;因此,配方的肿胀是负责抑制咪康唑通过皮肤的渗透。
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